公开(公告)号：US10351575B2

公开(公告)日：2019-07-16

申请号：US14442609

申请日：2013-11-13

Applicant: Array BioPharma Inc.

Inventor： Shelley Allen ,  Steven Wade Andrews ,  James F. Blake ,  Barbara J. Brandhuber ,  Julia Haas ,  Yutong Jiang ,  Timothy Kercher ,  Gabrielle R. Kolakowski ,  Allen A. Thomas ,  Shannon L. Winski

IPC: C07D401/14 ,  C07D491/048 ,  C07D405/14 ,  C07D231/40 ,  C07D231/54 ,  C07D401/12 ,  C07D403/02 ,  C07D403/04 ,  C07D403/14 ,  C07D405/12 ,  C07D413/12 ,  C07D453/02 ,  C07D231/52 ,  C07D231/56 ,  C07D401/04 ,  C07D409/14 ,  C07D471/08

Abstract: Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.

公开(公告)号：US20190144444A1

公开(公告)日：2019-05-16

申请号：US16191190

申请日：2018-11-14

Applicant: Mirati Therapeutics, Inc. ,  Array BioPharma Inc.

Inventor： James F. Blake ,  Laurence E. Burgess ,  Mark Joseph Chicarelli ,  James Gail Christensen ,  Adam Cook ,  Jay Bradford Fell ,  John P. Fischer ,  Matthew Arnold Marx ,  Macedonio J. Mejia ,  Pavel Savechenkov ,  Guy P.A. Vigers ,  Christopher Ronald Smith ,  Martha E. Rodriguez

IPC: C07D471/04 ,  C07D491/08 ,  A61P35/00

Abstract: The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.

公开(公告)号：US10125134B2

公开(公告)日：2018-11-13

申请号：US15814279

申请日：2017-11-15

Applicant: Mirati Therapeutics, Inc. ,  Array BioPharma Inc.

Inventor： James F. Blake ,  Laurence E. Burgess ,  Mark Joseph Chicarelli ,  James Gail Christensen ,  Jay Bradford Fell ,  John P. Fischer ,  John J. Gaudino ,  Erik James Hicken ,  Ronald Jay Hinklin ,  Matthew Randolf Lee ,  Matthew Arnold Marx ,  Macedonio J. Mejia ,  Martha E. Rodriguez ,  Pavel Savechenkov ,  Tony P. Tang ,  Guy P. A. Vigers ,  Henry J. Zecca

IPC: C07D471/04 ,  C07D519/00 ,  A61K31/519

Abstract: The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.

公开(公告)号：US10047097B2

公开(公告)日：2018-08-14

申请号：US15860948

申请日：2018-01-03

Applicant: Array BioPharma, Inc.

Inventor： Julia Haas ,  Steven W. Andrews ,  Yutong Jiang ,  Gan Zhang

IPC: C07D487/04 ,  C07D471/04 ,  C07D519/00 ,  A61K45/06 ,  A61K31/519 ,  A61K31/5377 ,  A61K9/00

Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.

公开(公告)号：US09790206B2

公开(公告)日：2017-10-17

申请号：US14770035

申请日：2014-02-27

Applicant: Array BioPharma Inc.

Inventor： C. Todd Eary ,  Bruno P. Hache ,  Derrick Juengst ,  Stacey Renee Spencer ,  Peter J. Stengel ,  Daniel John Watson

IPC: C07D403/12 ,  C07D231/56

CPC classification number: C07D403/12 ,  C07D231/56

Abstract: Provided herein are novel processes for preparing a compound of Formula (I) to the use of said compound as an intermediate in novel processes for the synthesis of indazole derivatives, and to indazole intermediates and derivatives prepared by the processes described herein.

公开(公告)号：US09763941B2

公开(公告)日：2017-09-19

申请号：US15179190

申请日：2016-06-10

Applicant: Array BioPharma, Inc.

Inventor： Daya Verma ,  Yogita Krishnamachari ,  Xiaohong Shen ,  Hanchen Lee ,  Ping Li ,  Rajinder Singh ,  LayChoo Tan

IPC: A61K31/506 ,  A61K9/20 ,  A61K9/48 ,  A61K9/00

CPC classification number: A61K31/506 ,  A61K9/0053 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2031 ,  A61K9/282 ,  A61K9/284 ,  A61K9/2866 ,  A61K9/485 ,  A61K9/4858 ,  A61K9/4866

Abstract: This invention relates to solid oral pharmaceutical formulations of (S)-methyl (1-((4-(3-(5-chloro-2-fluoro-3-(methyl -sulfonamido)phenyl)-1-isopropyl-1H-pyrazol-4-yl)pyrimidin-2-yl)amino)propan-2-yl)carbamate (COMPOUND A) and the use of these formulations for treating proliferative diseases, such as solid tumor diseases.

公开(公告)号：US20170247337A1

公开(公告)日：2017-08-31

申请号：US15593064

申请日：2017-05-11

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： David Askin ,  Chong Han ,  Jonathan W. Lane ,  Travis Remarchuk ,  Sagar Shakya ,  C. Gregory Sowell ,  Keith L. Spencer ,  Peter J. Stengel

IPC: C07D239/42

CPC classification number: C07D239/42 ,  C07D239/30 ,  C07D239/70 ,  C07D403/04

Abstract: The invention provides processes for preparing a compound of formula I and salts thereof, wherein R1 is defined herein, and compounds and intermediates of said formula.

公开(公告)号：US09693989B2

公开(公告)日：2017-07-04

申请号：US14034361

申请日：2013-09-23

Applicant: ARRAY BIOPHARMA, INC.

Inventor： Joseph P. Lyssikatos ,  Julie Marie Hicks ,  Fredrik P. Marmsater ,  Qian Zhao

IPC: A61K31/337 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D519/00 ,  A61K31/513 ,  A61K31/517 ,  A61K39/395

CPC classification number: A61K31/337 ,  A61K31/513 ,  A61K31/517 ,  A61K39/3955 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D519/00

Abstract: This invention provides compounds of Formula I wherein B, G, A, E, R1, R2, R3, m and n are as defined herein, which are useful as type I receptor tyrosine kinase inhibitors, and methods of use thereof in the treatment of hyperproliferative disorders in mammals.

公开(公告)号：US20170087156A1

公开(公告)日：2017-03-30

申请号：US15311148

申请日：2015-05-14

Applicant: Array BioPharma Inc.

Inventor： Shelley Allen ,  Steven W. Andrews ,  Brian Baer ,  Zackary Crane ,  Weidong Liu ,  Daniel John Watson

IPC: A61K31/506 ,  A61K9/00 ,  C07D207/16 ,  C07D403/14 ,  A61K45/06

CPC classification number: A61K31/506 ,  A61K9/0053 ,  A61K45/06 ,  C07D207/16 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14

Abstract: Provided is Compound (I) or a pharmaceutically acceptable salt thereof, which is an inhibitor of TrkA kinase and is useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation and inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis, pelvic pain syndrome, diseases related to an imbalance of the regulation of bone remodeling, and diseases resulting from Connective Tissue Growth Factor aberrant signaling.

公开(公告)号：US09598376B2

公开(公告)日：2017-03-21

申请号：US15053441

申请日：2016-02-25

Applicant: Novartis AG ,  Array BioPharma, Inc.

Inventor： Christoph Max Krell ,  Marian Misun ,  Daniel Andreas Niederer ,  Werner Heinz Pachinger ,  Marie-Christine Wolf ,  Daniel Zimmermann ,  Weidong Liu ,  Peter J. Stengel ,  Paul Nichols

IPC: C07D235/08 ,  C07D235/06 ,  A61K47/26 ,  A61K47/38 ,  A61K9/20 ,  C30B7/08 ,  C30B29/54 ,  A61K47/02 ,  A61K47/12

CPC classification number: A61K31/4184 ,  A61K9/0053 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K45/06 ,  A61K47/02 ,  A61K47/12 ,  A61K47/26 ,  A61K47/38 ,  C07B2200/13 ,  C07D235/06 ,  C07D235/08 ,  C30B7/08 ,  C30B29/54

Abstract: The present invention relates to processes for preparing 6-(4-bromo-2-fluorophenylamino)-7-fluoro -3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide, processes for preparing crystallized 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide, and intermediates useful therefore. Also provided herein are pharmaceutical compositions comprising this crystallized compound.